Indacaterol is a novel, ultra-long-acting, rapid onset β(2)-adrenoceptor agonist developed for Novartis for the once-daily management of asthma and chronic obstructive pulmonary disease. It was approved by the European Medicines Agency (EMA) on 30 November 2009 and by the FDA on 1 July 2011. Indacaterol is provided as its maleate salt form. Indacaterol is also a chiral molecule but only the pure R-enantiomer is dispensed.
02 Indacaterol powder (312753-06-3) video
03 Indacaterol powder Base Information
|Molecular Weight||392.499 g/mol|
|Appearance||Light Yellow Solid|
|Half Life||40 to 56 hours|
|Solubility||Soluble in DMSO (Slightly), Methanol (Slightly),Water Solubility 0.00798 mg/mL|
|Storage Condition||Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).|
|Application||Indacaterol is a β-adrenoreceptor agonists for treatment of asthma and bronchodilator treatment for patients with chronic obstructive pulmonary diseases.|
04 Indacaterol powder General Description
Indacaterol powder is a long-acting bronchodilator. Bronchodilators are medicines that are breathed in through the mouth to open up the bronchial tubes (air passages) in the lungs. They relieve cough, wheezing, shortness of breath, and troubled breathing by increasing the flow of air through the bronchial tubes.
Indacaterol powder is a monohydroxyquinoline that consists of 5-[(1R)-2-amino-1-hydroxyethyl]-8-hydroxyquinolin-2-one having a 5,6-diethylindan-2-yl group attached to the amino function. Used as the maleate salt for treatment of chronic obstructive pulmonary disease. It has a role as a beta-adrenergic agonist and a bronchodilator agent. It is a quinolone, a monohydroxyquinoline, a member of indanes, a secondary alcohol and a secondary amino compound. It is a conjugate base of an indacaterol(1+).
05 Indacaterol (312753-06-3) History
Indacaterol is used to treat air flow blockage and prevent worsening of chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema. COPD is a long-term lung disease that causes bronchospasm (wheezing or difficulty with breathing).
A Phase III trial published in March 2010 examined the efficacy and safety of indacaterol in COPD patients. This study, conducted in the U.S., New Zealand, and Belgium, compared indacaterol dry-powder inhaler to placebo in 416 COPD patients, mostly moderate to severe (mean FEV1 of 1.5 L). Indacaterol produced statistically improved FEV1 (both trough and AUC) and decreased use of rescue medication compared to placebo, but with safety and tolerability similar to those of placebo.
A year-long, placebo-controlled trial published in July 2010 suggests indacaterol may be significantly more effective than twice-daily formoterol in improving FEV1. There were some reductions in the need for rescue medication, but these were not significantly different; nor was there any difference in the rate of exacerbation between the 2 active treatments.
A study published in October, 2011 in the European Respiratory Journalcompared indacaterol with tiotropium over the study period of 12 weeks.The study found no statistical difference between the effects of the two drugs on FEV1. Indacaterol yielded greater improvements in transition dyspnoea index (TDI) total score and St. George’s Respiratory Questionnaire (SGRQ) total score.
A recent Cochrane Library meta-analysis indicates that the clinical benefit in lung function from indacaterol is at least as good as that seen withtwice-daily long-acting beta2-agonists.
06 Indacaterol (312753-06-3) Mechanism Of Action
Indacaterol works by stimulating adrenergic beta-2 receptors in the smooth muscle of the airways. This causes relaxation of the muscle, thereby increasing the diameter of the airways, which become constricted in asthma and COPD. It is also long acting due to its high affinity to the lipid raft domains in the airway membrane so it slowly dissociates from the receptors. Indacaterol also has a high intrinsic efficacy so it is also very rapid acting – onset of action occurs within 5 minutes.
The pharmacological effects of beta2-adrenoceptor agonist drugs, including indacaterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3’, 5’-adenosine monophosphate (cyclic monophosphate). Increased cyclic AMP levels cause relaxation of bronchial smooth muscle. In vitro studies have shown that indacaterol has more than 24-fold greater agonist activity at beta2-receptors compared to beta1-receptors and 20-fold greater agonist activity compared to beta3-receptors. This selectivity profile is similar to formoterol. The clinical significance of these findings is unknown.
07 Indacaterol (312753-06-3) Application
Indacaterol is used to treat trouble breathing and wheezing due to a certain ongoing lung disease (chronic obstructive pulmonary disease-COPD, including chronic bronchitis and/or emphysema). It is used if your breathing problems are not controlled with other medication (such as a quick-relief inhaler). It works in the airways by relaxing muscles and openingair passages to improve breathing.
This medication should not be used for severe/sudden breathing problems. Other medications, such as a quick-relief inhaler should be used instead of indacaterol for sudden breathing problems. This medication is not a substitute for corticosteroids (such as beclomethasone, fluticasone, prednisone).
Indacaterol is an effective treatment for patients with stable COPD; it offers benefits that are clinically similar to those of existing twice-daily preparations within the same class of medication but provides the possibleadvantage of once-daily dosing.
08 Indacaterol (312753-06-3) More research
Indacaterol serum concentrations declined in a multi-phasic manner withan average terminal half-life ranging from 45.5 to 126 hours. The effective half-life, calculated from the accumulation of indacaterol after repeated dosing with once daily doses between 75 mcg and 600 mcg ranged from 40 to 56 hours which is consistent with the observed time-to-steadystate of approximately 12-15 days.
09 Indacaterol (312753-06-3) Document Download
10 Indacaterol (312753-06-3) Reference
 Naline E, Trifilieff A, Fairhurst RA, Advenier C, Molimard M: Effect of indacaterol, a novel long-acting beta2-agonist, on isolated human bronchi. Eur Respir J. 2007 Mar;29(3):575-81. Epub 2006 Nov 29.
 Kagan M, Dain J, Peng L, Reynolds C: Metabolism and pharmacokinetics of indacaterol in humans. Drug Metab Dispos. 2012 Sep;40(9):1712-22. doi: 10.1124/dmd.112.046151. Epub 2012 May 30.
 Reid DJ, Pham NT: Emerging Therapeutic Options for the Management of COPD. Clin Med Insights Circ Respir Pulm Med. 2013 Apr 9;7:7-15. doi: 10.4137/CCRPM.S8140. Print 2013.
 European Public Assessment Report for Onbrez BreezhalerArchived 2010-01-16 at the Wayback Machine.
- 01. Overview
- 02. Indacaterol powder (312753-06-3) video
- 03. Indacaterol powder Base Information
- 04. Indacaterol powder General Description
- 05. Indacaterol (312753-06-3) History
- 06. Indacaterol (312753-06-3) Mechanism Of Action
- 07. Indacaterol (312753-06-3) Application
- 08. Indacaterol (312753-06-3) More research
- 09. Indacaterol (312753-06-3) Document Download
- 10. Indacaterol (312753-06-3) Reference